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N-alkyl-4-methyleneamino-3-hydroxy-2-pyridones

a technology of alkyl-4-methyleneamino-3-hydroxy-2-pyridone and alkyl-4-methyleneamino-3-hydroxy-2-pyridone, which is applied in the direction of biocide, antibacterial agents, drug compositions, etc., can solve the problem that only a small number of antimicrobials are produced that are truly clinically acceptabl

Active Publication Date: 2004-05-20
AERPIO TERAPYUTIKS INK
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

0134] Except as otherwise noted, the articles "a", "an", and "the" mean "one or more".

Problems solved by technology

Indeed, few antimicrobials are produced that are truly clinically-acceptable in term of their spectrum of antimicrobial activity, avoidance of microbial resistance, and pharmacology.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

examples 1-38

C. EXAMPLES 1-38

[0094] Examples are prepared in accordance with the above method by varying the amine.

1 11 Example R1 X 1 12 13 2 14 15 3 16 17 4 18 19 5 20 21 6 22 23 7 24 25 8 26 27 9 28 29 10 30 31 11 32 33 12 34 35 13 36 37 14 38 39 15 40 41 16 42 43 17 44 45 18 46 47 19 48 49 20 50 51 21 52 53 22 54 55 23 56 57 24 58 59 25 60 61 26 62 63 27 64 65 28 66 67 29 68 69 30 70 71 31 72 73 32 74 75 33 76 77 34 78 79 35 80 81 36 82 83 37 84 85 38 86 87

example 1

1-Benzyl-3-Hydroxy-4-piperidin-1-ylmethyl-1H-pyridin-2-one

[0095] .sup.1H NMR (300 MHz, CD.sub.3OD) .delta. 1.81 (m, 6H), 3.07 (m, 2H), 3.51 (m, 2H), 4.23 (s, 2H), 5.24 (s, 2H), 6.31 (d, J=6.9 Hz, 1H), 7.35 (m, 6H); .sup.19F NMR (252 MHz, CD.sub.3OD) .delta. 85.5; 13C NMR (75 MHz, DMSO) .delta. 21.3, 22.7, 51.8, 52.5, 53.1, 106.4, 117.4, 127.7, 128.0, 128.2, 128.9, 137.3, 147.4, 158.0; ES MS(M+1) 299.12; HRMS Calcd. For C.sub.18H.sub.22N.sub.2O.sub.2, 298.38. Found (M+1) 299.17.

example 2

1-Benzyl-3-Hydroxy-4-morpholin-1-ylmethyl-1H-pyridin-2-one

[0096] .sup.1H NMR (300 MHz, DMSO) .delta. 3.25 (m, 4H), 3.81 (m, 4H), 4.18 (s, 2H), 5.17 (s, 2H), 6.31 (d, J=6.9 Hz, 1H), 7.35 (m, 6H); .sup.19FNMR (300 MHz, DMSO) .delta. 88.5; .sup.13C NMR (300 MHz, DMSO) .delta. 51.6, 51.8, 53.4, 63.5, 107.9, 119.1, 127.8, 128.0, 128.2, 128.9, 137.3, 147.5, 158.3; ES MS(M+1) 301.12; HRMS Calcd. For C.sub.17H.sub.20N.sub.2O.sub.3, 300.35.

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Abstract

Compounds of Formula (I) are effective in the treatment of a microbial infection.

Description

[0001] This application claims priority under Title 35, United States Code 119(e) from U.S. Provisional Application Serial No. 60 / 425,070 filed Nov. 9, 2002, incorporated herein by reference.[0002] The invention is directed certain N-alkyl-4-methyleneamino-3-hydrox-y-2-pyridones useful as antimicrobials.BACKGROUND OF INVENTION[0003] The chemical and medical literature describes compounds that are said to be antimicrobial, i.e., capable of destroying or suppressing the growth or reproduction of microorganisms, such as bacteria. For example, such antibacterials and other antimicrobials are described in Antibiotics, Chemotherapeutics, and Antibacterial Agents for Disease Control (M. Grayson, editor, 1982), and E. Gale et al., The Molecular Basis of Antibiotic Action 2d edition (1981).[0004] The mechanism of action of these antibacterials vary. One notable mechanism is bacterial aminopeptidase (bMAP) inhibitors. bMAP inhibition is an important therapeutic target in anti-infective focus ...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61P31/00C07D213/69C07D401/06C07D401/12C07D401/14C07D405/12C07D417/06C07D491/10
CPCC07D213/69C07D401/06C07D401/12C07D491/10C07D405/12C07D417/06C07D401/14A61P31/00A61P31/04
Inventor WARSHAKOON, NAMAL CHITHRANGABUSH, RODNEY DEAN
Owner AERPIO TERAPYUTIKS INK
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